- Diversity oriented approach to polycyclic compounds through the diels-alder reaction and the Suzuki coupling
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A diversity oriented strategy has been demonstrated to deliver small "drug like" molecules using alkylation, Diels-Alder reaction, and Suzuki-Miyaura cross-coupling as key steps. This methodology allows access a wide range of molecules using simple scaffolds such as indanes, tetralins and tetrahydroisoquinolines, which can enhance the chemical space for potential therapeutic molecules.
- Kotha, Sambasivarao,Misra, Shilpi,Srinivas, Venu
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scheme or table
p. 4052 - 4062
(2012/09/07)
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- Inhibitors of phenylalanine ammonia-lyase: Substituted derivatives of 2-aminoindane-2-phosphonic acid and 1-aminobenzylphosphonic acid
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Six derivatives of 2-aminoindane-2-phosphonic acid and 1-aminobenzylphosphonic acid were synthesized. The compounds were tested both as inhibitors of buckwheat phenylalanine ammonia-lyase (in vitro) and as inhibitors of anthocyanin biosynthesis (in vivo). (±)-2-Amino-4-bromoindane-2-phosphonic acid was found to be the strongest inhibitor from investigated compounds. The results obtained are a basis for design of phenylalanine ammonia-lyase inhibitors useful in the enzyme structure studies in photo labelling experiments.
- Miziak, Piotr,Zon, Jerzy,Amrhein, Nikolaus,Gancarz, Roman
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p. 407 - 415
(2007/10/03)
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- Structure and Reactivity of Isoannulated Heterocyclic Systems with 4n-? and (4n + 2)-? Electrons, XVIII. - Benzothiophenes with Symmetric Structure: Modified and Optimized Preparations by the S-Oxide Route
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Benzothiophenes (15) with symmetric structure have been prepared efficiently from 1,3-dihydrobenzothiophene 2-oxides (9) by reaction with aluminium oxide, by O-acylation with trifluoroacetic anhydride, or O-alkylation with methyl trifluoromethanesulfonate.The aromatization of the S-oxides 9 is achieved by O-functionalization, subsequent elimination, and consecutive deprotonation.
- Kreher, Richard P.,Kalischko, Juergen
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p. 645 - 654
(2007/10/02)
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- Studies on the Chemistry of Isoindoles and Isoindolenines, XXXI. 4,5,6,7-Tetrachloro-and 4,5,6,7-Tetrabromo-2H-isoindoles
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The crystalline 2H-isoindoles 4b are synthesized starting with substituted 2-methylsulfonyl-2,3-dihydro-1H-isoindoles 3 by base-induced elimination of methanesulfinic acid.Compared with the parent compound, a considerable thermal stabilization and chemical deactivation is caused by the halogen atoms at the carbocyclic system.The spectroscopic properties of the o-quinonoid hetarenes 4b have been investigated.
- Kreher, Richard P.,Herd, Karl Josef
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p. 1827 - 1832
(2007/10/02)
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